title: Chitosan/pectin polyelectrolyte complexes: selection of suitable preparative conditions for colon-specific delivery of vancomycin.
abstract: The influence of polyelectrolyte complexes composed of chitosan and pectin on the release behaviour of vancomycin has been investigated. Polyelectrolyte complexes between chitosan and pectin were prepared in various pH regions and at different molar ratios by mixing solutions of pectin and chitosan with the same ionic strength. The precipitates were collected by spray-drying and tablets were obtained with the different complexes and vancomycin. FT-IR spectra and TGA thermograms were analysed to study the degree of interactive strength between polyions. In vitro swelling, mucoadhesion and release tests were performed in order to investigate the chitosan/pectin complex ability in the delivery of vancomycin in the gastro-intestinal tract. The results confirmed the formation of polyelectrolyte complexes between pectin and chitosan at pH values in the vicinity of the pKa interval of the two polymers. Chitosan/pectin complexes showed a pH-sensitive swelling ability and drug release behaviour suggesting their possible use for colon-specific localization of vancomycin. Among the different complexes, chitosan/pectin complex prepared in molar ratio of 1:9 showed the highest mucoadhesive properties and a pH-dependent swelling sensitivity suitable for colon-delivery. Moreover, the particular composition of these complexes improved vancomycin availability at alkaline pH on the bases of an enzyme-dependent degradation as confirmed from release studies performed in presence of beta-glucosidase.
authors.affiliation: Department of Pharmaceutical Sciences, Bologna University, Bologna, Italy. federica.bigucci@unibo.it
authors.forename: F
authors.initials: F
authors.lastname: Bigucci
authors.forename: B
authors.initials: B
authors.lastname: Luppi
authors.forename: T
authors.initials: T
authors.lastname: Cerchiara
authors.forename: M
authors.initials: M
authors.lastname: Sorrenti
authors.forename: G
authors.initials: G
authors.lastname: Bettinetti
authors.forename: L
authors.initials: L
authors.lastname: Rodriguez
authors.forename: V
authors.initials: V
authors.lastname: Zecchi
mesh_terms: D000268:Adhesiveness; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical; D048271:Chitosan / Q000737:chemistry*; D003106:Colon / Q000187:drug effects*; D003890:Desiccation; D004339:Drug Compounding; D016503:Drug Delivery Systems; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D007413:Intestinal Mucosa / Q000378:metabolism; D008970:Molecular Weight; D010368:Pectins / Q000737:chemistry*; D011108:Polymers; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013552:Swine; D013607:Tablets; D013818:Thermogravimetry; D014640:Vancomycin / Q000008:administration & dosage* / Q000493:pharmacokinetics
chemical_list: D000900:Anti-Bacterial Agents; D011108:Polymers; D013607:Tablets; D014640:Vancomycin; D010368:Pectins; D048271:Chitosan